JMV 2959 hydrochloride|2448414-54-6|-陌孚医药/Medlife

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JMV 2959 hydrochloride

目录号: PL06143 纯度: ≥98%

CAS No. :2448414-54-6

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中文名称	JMV 2959 hydrochloride
中文别名	化合物JMV 2959 HYDROCHLORIDE
英文名称	JMV 2959 hydrochloride
英文别名	HY-U00433A;MS-30006;JMV 2959 hydrochloride (925238-89-7 free base);JMV2959hydrochloride;JMV 2959 HCl ;JMV-2959 HCl ;JMV2959 HCl ;JMV-2959 hydrochloride ;JMV2959 hydrochloride;AKOS040733498;JMV 2959 (hydrochloride);JMV 2959 hydrochloride;CS-0062683;BCP30096;2448414-54-6;JMV2959HCL;JMV 2959 hydrochloride (925238897 free base),JMV 2959 hydrochloride (925238 89 7 free base)
Cas No.	2448414-54-6
分子式	C₃₀H₃₃ClN₆O₂
分子量	545.08
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	JMV 2959 hydrochloride 是一种生长激素促分泌素受体 1a 型 (GHS-R_1a) 拮抗剂，作用于 LLC-PK₁ 细胞，抑制 GHS-R_1a，IC₅₀ 值为 32±3 nM。
生物活性	JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R 1a ) antagonist with an IC 50 of 32±3 nM in LLC-PK 1 cells.
性状	Solid
IC50 & Target[1][2]	IC50: 32±3 nM (GHS-R1a, in LLC-PK1 cells)
体外研究(In Vitro)	JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself. The dissociation constant of the receptor/JMV 2959 complex is determined by the Schild method. This experiment reveals a dissociation constant Kb of 19±6 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Intraperitoneal (i.p.) administration of Ghrelin (0.033, 0.1, and 0.33 mg/kg) does not alter the acoustic startle responses (ASR) or prepulse inhibition (PPI) in rats. Conversely, i.p. injection of JMV 2959 (1, 3, and 6 mg/kg), dose dependently decrease the ASR and increase PPI. Pretreatment with JMV 2959 at a dose with no effect on ASR or PPI per se, completely blocks Phencyclidine (PCP)-induced (2 mg/kg) deficits in PPI while pretreatment with the highest dose of Ghrelin does not potentiate or alter PPI responses of a sub-threshold dose of PCP (0.75 mg/kg). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Moulin A, et al. The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist. Amino Acids. 2013 Feb;44(2):301-14. [2]. Engel JA, et al. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. Psychopharmacology (Berl). 2015 Dec;232(23):4285-92.

溶解度数据	In Vitro: DMSO : 250 mg/mL (458.65 mM; Need ultrasonic)H₂O : 25 mg/mL (45.86 mM; Need ultrasonic)配制储备液

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